Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved FRET binding assay

  • J Med Chem. 2015 Mar 12;58(5):2547-52. doi: 10.1021/jm501395b.
Iuliia A Karpenko  1 ,  Jean-François Margathe ,  Thiéric Rodriguez ,  Elsa Pflimlin ,  Elodie Dupuis ,  Marcel Hibert ,  Thierry Durroux ,  Dominique Bonnet
Affiliations
  • 1. Laboratoire d'Innovation Thérapeutique, UMR7200 CNRS/Université de Strasbourg, Labex MEDALIS, Faculté de Pharmacie , 74 route du Rhin, 67401 Illkirch, France.
PMID: 25642985 DOI: 10.1021/jm501395b
Abstract

The design and the synthesis of the first high-affinity fluorescent ligands for Oxytocin Receptor (OTR) are described. These compounds enabled the development of a TR-FRET based assay for OTR, readily amenable to high throughput screening. The validation of the assay was achieved by competition experiments with both peptide and nonpeptide OTR ligands as competitors. These probes represent the first selective fluorescent ligands for the oxytocin G protein-coupled receptor.